化学名称 : PI 103 盐酸盐
CAS : 371935-74-9
英文名称: PI103 hydrochloride
英文同义词: 3-[4-(4-Morpholinylpyrido[3',2':4,5]f uro[3,2-d]pyrimidin-2-yl]phenol hydrochloride;PI 103 HYDROCHLORIDE
溶解度:Soluble in DMSO
储存条件:-20C 2 years
生物活性
A selective class I PI3K inhibitor; it inhibits PI3K p110 isoforms, mTOC1 and also DNA-PK; a valuable tool compound.Inhibitor of DNA-PK, PI 3-kinase (p110α) and mTOR (IC50 values are 2, 8, 20, 26, 48, 83, 88, 150, 850, 920, ~ 1000 and 2300 nM for DNA-PK, p110α, mTORC1, PI3KC2β, p110δ, mTORC2, p110β, p110γ, ATR, ATM, PI3KC2α and hsVPS34 respectively). Inhibits growth of human tumor xenografts in mice in vivo.
参考文献
Fan et al (2006) A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer cell 9 341. Knight et al (2006) A pharmacological map of the PI3-K family defines a role for p110a in insulin signaling. Cell 125 733. Raynaud et al (2007) Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositol 3-kinase. Cancer Res. 67 5840.